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咪唑并[4,5-c]喹啉作为PI3K/PKB信号通路的抑制剂

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

作者信息

Stauffer Frédéric, Maira Sauveur-Michel, Furet Pascal, García-Echeverría Carlos

机构信息

Novartis Institute for BioMedical Research, Oncology Drug Discovery, Klybeckstrasse 141, Postfach, CH-4002 Basel, Switzerland.

出版信息

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1027-30. doi: 10.1016/j.bmcl.2007.12.018. Epub 2007 Dec 15.

Abstract

Imidazo[4,5-c]quinoline derivatives have been discovered and developed as potent and effective modulators of the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) pathway to lead to clinical development candidates. The SAR data of representative examples of this compound class and their biological profiling in cellular and in vivo settings are presented and discussed.

摘要

咪唑并[4,5-c]喹啉衍生物已被发现并开发为磷脂酰肌醇3-激酶(PI3K)/蛋白激酶B(PKB)途径的有效调节剂,从而产生临床开发候选药物。本文展示并讨论了这类化合物代表性实例的构效关系数据及其在细胞和体内环境中的生物学特性分析。

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